Physostigmine (Synonyms: Physostigmine; Eserine; Antilirium; Physostol; Esromiotin; Ezerin;) |
Catalog No.GB62186
One-Click Copy Product Info
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Physostigmine is a reversible acetylcholinesterase (AChE) inhibitor that rapidly crosses cell membranes, penetrates the blood-brain barrier, and stimulates central cholinergic neurotransmission.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 57-47-6
Sample solution is provided at 25 µL, 10mM.
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Physostigmine is a reversible acetylcholinesterase (AChE) inhibitor that rapidly crosses cell membranes, penetrates the blood-brain barrier, and stimulates central cholinergic neurotransmission[1,2].Acetylcholinesterase is responsible for breaking down utilized acetylcholine. By interfering with acetylcholine metabolism, Physostigmine indirectly stimulates nicotinic and muscarinic receptors, leading to an increase in available acetylcholine at the synapse. Physostigmine is commonly used in research on cholinergic signaling pathways and related disease models, as well as in the treatment of glaucoma and anticholinergic toxicity[3, 4].
In vitro, Physostigmine (0.2-2μM) was incubated with erythrocyte AChE from human, rhesus monkey, swine, and guinea pig, and the enzyme inhibition curve was continuously monitored for 30min to calculate the bimolecular inhibition rate constant (ki), and the inhibition constants showed minimal variation across species (Human: 5.40 × 106M-1 min-1; Rhesus monkey: 6.34 × 106M-1 min-1; Swine: 4.14 × 106M-1 min-1; Guinea pig: 3.50 × 106M-1 min-1 )[5]. Incubation of Physostigmine (1mM) with serum from humans with normal liver function for 120min partially inhibited the deacylation process of acylated ghrelin (AG) in the serum, resulting in a significantly higher residual level of AG after incubation compared to the control group[6].
In vivo, immediate administration of Physostigmine (0.1mg/kg) via intraperitoneal injection to mice after hypoxic exposure (FiO2 = 0.1) significantly improved the mice's short-term memory performance in the novel object recognition test, preventing the cognitive decline induced by hypoxia[7]. Subcutaneous injection of Physostigmine (0.4mg/kg) administered 15min before behavioral testing in C57BL/6J mice significantly reduced the peak startle amplitude in response to a 120dB acoustic stimulus and prolonged the time to reach the peak amplitude[8]. Treatment of a cecal ligation and puncture (CLP)-induced sepsis mouse model with Physostigmine (80μg/kg; 3 times/day; 3 days; i.p.) significantly improved the survival rate of the mice[9].
References:
[1] ARENS A M, SHAH K, AL-ABRI S, et al. Safety and effectiveness of physostigmine: a 10-year retrospective review[J]. Clinical Toxicology, 2018, 56(2): 101-107.
[2] ARENS A M, KEARNEY T. Adverse effects of physostigmine[J]. Journal of Medical Toxicology, 2019, 15(3): 184-191.
[3] TRIGGLE D J, FILLER R. The pharmacology of physostigmine[J]. CNS Drug Reviews, 1998, 4: 87-136.
[4] RUMACK B H. Anticholinergic poisoning: treatment with physostigmine[J]. Pediatrics, 1973, 52(3): 449-451.
[5] HERKERT N M, THIERMANN H, WOREK F. In vitro kinetic interactions of pyridostigmine, physostigmine and soman with erythrocyte and muscle acetylcholinesterase from different species[J]. Toxicology Letters, 2011, 206(1): 41-46.
[6] MURAKAMI K, TAKIGUCHI S, MIYAZAKI Y, et al. Perturbation of acyl ghrelin profile after liver transplantation[J]. Journal of Surgical Research, 2015, 199(2): 450-457.
[7] BEKKER A, HAILE M, GINGRICH K, et al. Physostigmine reverses cognitive dysfunction caused by moderate hypoxia in adult mice[J]. Anesthesia & Analgesia, 2007, 105(3): 739-743.
[8] CLARK M G, SUN W, MYERS T M, et al. Effects of physostigmine and human butyrylcholinesterase on acoustic startle reflex and prepulse inhibition in C57BL/6J mice[J]. Pharmacology Biochemistry and Behavior, 2005, 81(3): 497-505.
[9] HOFER S, EISENBACH C, LUKIC I K, et al. Pharmacologic cholinesterase inhibition improves survival in experimental sepsis[J]. Critical Care Medicine, 2008, 36(2): 404-408.
| Cell experiment [1]: | |
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Cell lines |
Serum from patients with normal liver |
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Preparation Method |
Serum from patients with normal liver was incubated with synthetic ghrelin for 120min at 37℃ in the absence or presence of 1mM Physostigmine, in final volume of 400μL. The incubation was stopped by the addition of 1N HCl (final concentration of 10%) and by setting the sample on ice. After incubation, AG was immediately measured using an ELISA assay. |
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Reaction Conditions |
1mM; 120min |
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Applications |
Physostigmine treatment partially inhibited the deacylation process of AG in serum, resulting in a significantly higher residual amount of AG after incubation compared to the control group. |
| Animal experiment [2]: | |
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Animal models |
CLP-induced septic C57BL/6 mice |
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Preparation Method |
Immediately after CLP-induced sepsis, mice were treated with Physostigmine (80μg/kg; i.p.) three times daily for 3 days. Survival after CLP was assessed four to six times a day for ≥ 7 days. |
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Dosage form |
80μg/kg; 3 times/day; 3 days; i.p. |
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Applications |
Physostigmine treatment significantly improved the survival rate of CLP-induced sepsis mice. |
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References: |
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| Cas No. | 57-47-6 | SDF | |
| Synonyms | Physostigmine; Eserine; Antilirium; Physostol; Esromiotin; Ezerin; | ||
| Canonical SMILES | CN1[C@](N(C)CC2)([H])[C@]2(C)C3=C1C=CC(OC(NC)=O)=C3 | ||
| Formula | C15H21N3O2 | M.Wt | 275.35 |
| Solubility | DMSO : 50 mg/mL (181.59 mM; Need ultrasonic) | Storage | Store at-20℃ |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.6317 mL | 18.1587 mL | 36.3174 mL |
| 5 mM | 726.3 μL | 3.6317 mL | 7.2635 mL |
| 10 mM | 363.2 μL | 1.8159 mL | 3.6317 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)